Prostatic cancer (prostatic carcinoma, abbreviated as PCa) is the most common malignant neoplasm in in male reproductive system. The incidence thereof increases with age, and differs significantly from region to region, which is higher in U.S. and Europe. Second to lung cancer, prostatic cancer is the second cancer leading to death in men. In the past, prostatic cancer has not been paid attention in China, since it belongs to a small disease in the spectrum of tumor. However, with the social development and progress in our country, the aging of society, urbanization, westernization of dietary structure and advances in detection technology, the incidence of prostate cancer was significantly increased. A foreign survey about prostate cancer which was completed by The Second Hospital of Tianjin Medical University and Diagnosis and Treatment of Prostate cancer in Tianjin in 2011 showed that the incidence of prostate cancer in Tianjin was rapidly rising, the incidence of prostate cancer increased by 4 times in 20 years, and the number of patients with prostate cancer accounted for 13.4% of inpatient with urinary tract tumors. Prostatic cancer which was rare cancer in the past becomes common tumors. The incidence of prostate cancer has the same trend in China.
Androgen receptor is a ligand-dependent trans-transcriptional regulatory protein with 110,000 Dalton molecular weight. Androgen receptor plays a very important role in the pathogen and deterioration process of prostate cancer, and in male hormone-related diseases such as acne, male alopecia, and so on.
Traditional methods for treating prostate cancer include surgery or using androgen receptor antagonists such as bicalutamide (Casodex). However, patients will develop drug resistance after 2-4 years treatment, while bicalutamide has side effects of stimulating the proliferation of cancer, therefore patients must stop using bicalutamide. Recent studies have found that bicalutamide will activate androgen receptors, thereby stimulating the proliferation of cancer.
Therefore, there is still a need in the art to develop compounds having superior pharmacodynamic properties to prostatic cancer.